Topic:Benzimidazoles
Benzimidazoles are a class of anthelmintic compounds used to control parasitic infections in horses. These compounds are effective against a range of gastrointestinal nematodes by interfering with the parasites' energy metabolism. Common benzimidazoles used in equine medicine include fenbendazole, mebendazole, and oxibendazole. The efficacy of benzimidazoles can be influenced by factors such as dosage, administration frequency, and the presence of resistant parasite strains. Resistance to benzimidazoles is a growing concern in equine parasitology, necessitating ongoing research into resistance mechanisms and alternative control strategies. This page compiles peer-reviewed research studies and scholarly articles that explore the pharmacodynamics, resistance patterns, and clinical applications of benzimidazoles in horse health management.
Reduced efficacy of anthelmintics in young compared with adult horses. Studies on a Thoroughbred breeding farm in Ohio from 1982 to 1988 demonstrated the value of three anthelmintic pastes (ivermectin, oxibendazole, pyrantel pamoate) in controlling benzimidazole resistant cyathostomes (small strongyles) in adult horses. However, a comparison of drug efficacy in suppressing faecal egg counts for the full period between treatments showed a significant reduction in efficacy of all drugs in yearling horses compared with adults. Mean faecal egg counts of adult horses were generally kept below 100 eggs per gram (epg) of faeces when using oxibendazole or pyrantel pamoat...
A survey of equine parasite control practices in Tennessee. A weighted, random sample of 130 horse owners in Tennessee was selected from subscribers to an equine newsletter published by the Agricultural Extension Service. Data about the participants' farms, horses, parasite control practices, and sources of information regarding equine parasite control were obtained through a telephone survey. The response rate was 98%. The typical respondent kept 4 horses on 2 pastures totaling 15 acres, and did not rotate pastures as a parasite control measure. The majority (83%) of horse owners indicated that they administered anthelmintics according to a regular sc...
Emergence from inhibited development of cyathostome larvae in ponies following failure to remove them by repeated treatments with benzimidazole compounds. The effect of three albendazole treatments at 5-week intervals, beginning at turnout in April, on cyathostome infections in Shetland ponies was compared with the effect of sequential treatments with albendazole, oxfendazole and oxibendazole. The results showed a substantial reduction in faecal egg output after the first albendazole treatment. Since faecal egg counts remained very low, no estimation of the effect of the second treatment was possible. The third treatment with albendazole and oxibendazole was followed by an increase in faecal egg counts to values of greater than 100 eggs g-1 with...
Anthelmintic drug resistance in the UK. The term 'anthelmintic drug resistance' describes the heritable ability of some nematode parasites to survive treatment with anthelmintic drugs at the recommended therapeutic dose levels. Genes for resistance appear to be present in many of the important pathogenic nematodes of ruminants and horses. Under intensive management systems, where heavy reliance is placed on anthelmintic drugs for worm control, the selection of resistant genotypes may result in increased reports of the drugs failing to control the nematode populations against which they are aimed. Anthelmintic resistance has been rep...
Effectiveness of oxibendazole against benzimidazole-resistant strongyles in horses. Twenty-eight horses with a residual burden of strongyle eggs in the faces after treatment with mebendazole (MBZ) paste were treated with a suspension of either MBZ or oxibendazole (OBZ). Fecal samples were collected before and 14 days after these treatments. The number of strongyle eggs/g (epg) of feces for each horse was estimated using the Cornell-McMaster dilution and the Cornell-Wisconsin double centrifugation procedures. The epg for each horse was transformed using log (x + 1) and in an analysis of variance of the reduction in egg count for each horse on the logarithmic scale, there was a...
Critical and controlled tests of activity of a macrocyclic lactone (compound F28249-alpha) against natural infections in internal parasites of equids. Thirteen critical tests (n = 11 horses and 2 ponies) and 4 controlled tests (n = 4 donkeys and 6 horses) were performed to evaluate the activity of the experimental macrocyclic lactone compound F28249-alpha against internal parasites of equids. In the critical tests, activity was determined mainly against the large parasites, but 1 critical test also included benzimidazole-resistant small strongyles. In the controlled tests, evaluation of drug activity included large parasites and stomach worms in all 4 tests, and lungworms in 2 tests. The period between treatment and euthanasia was 6 to 9 day...
Oxfendazole: activity of a two-dose treatment regimen on natural infections of internal parasites of equids, with emphasis on migrating large strongyles in controlled tests in 1986 and 1987. Oxfendazole paste formulation was administered intraorally at a dosage of 10 mg/kg of body weight, twice (48 hours between treatments) in 5 controlled tests (experiments A, B, C, D, and E) to 18 equids (14 horses and 4 ponies) that were 5 to 24 months old in 1986 and 1987. Activity was evaluated against naturally acquired infections of various internal parasites, with emphasis on migratory stages of Strongylus vulgaris and S edentatus. The number of treated and nontreated equids in each experiment (horses in experiments A to D and ponies in experiment E) was: A, 1 and 1; B, 3 and 3; C, 3 and 1...
Experimental chemotherapy in horses infected with benzimidazole-resistant small strongyles. The presence of benzimidazole-resistant strains of equine small strongyles was confirmed in horses at two properties in north west England by a series of faecal egg counts and larval cultures after treatment with mebendazole. A trail formulation of mebendazole in combination with piperazine citrate gave greater reductions in faecal egg counts than mebendazole alone but was much less effective than pyrantel embonate or dichlorvos.
Piperazine resistance in population-B equine strongyles: a study of selection in Thoroughbreds in Kentucky from 1966 through 1983. Observations were completed over an 18-year period (1966 through 1983) in Thoroughbred mares (15/year) and yearlings (11 to 24/year) on a farm where benzimidazole-resistant small strongyles had emerged previously (1962 to 1965). This farm was operated as a closed, nonboarding type, which included a racing stable for its home-bred foals. At 2-week intervals, counts of worm eggs per gram of feces (EPG) and larvae per gram of feces were done to monitor strongyle infections and efficacies of bimonthly (every 8 weeks) antiparasitic treatments that were administered by stomach tube or were fed (dich...
Resistance of equine small strongyles to benzimidazoles in Belgium. The presence of benzimidazole resistant equine small strongyles was demonstrated in two Belgian studs. Egg reduction tests and in vitro egg hatch assays with thiabendazole and mebendazole were used.
Observations on equine strongyle control in southern temperate USA. A program of rotational anthelmintic treatments at eight-week intervals had failed to provide satisfactory equine strongyle control at a stable in southern USA. Anthelmintic resistance had rendered benzimidazoles ineffective, and intervals between treatments with other drugs were too great to prevent environmental contamination with ova. Ivermectin treatments at eight week intervals or pyrantel pamoate treatments at four week intervals successfully reduced egg counts for the majority of the summer grazing period. In southern temperate USA, translation of strongyle ova to larvae was most effici...
HPLC determination and pharmacokinetics of thiabendazole and its major metabolite 5-OH thiabendazole in equine plasma. Separate high performance liquid chromatographic methods were developed for thiabendazole (TBZ) and 5-hydroxy thiabendazole (5-OH-TBZ) determination in horse plasma using 1-methyl-2-phenyl benzimidazole (MPBZ) as an internal standard. In both methods TBZ and 5-OH-TBZ were extracted from plasma using organic solvents, injected on to a C-18 column, and eluents monitored by a fluorescence detector. However, mobile phase composition, extraction solvent as well as detector wavelength differed in the two methods. The linear range for TBZ was 0.02 to 0.77 microgram ml-1 while that for 5-OH-TBZ was 0....
Radioimmunoassay of detomidine, a new benzylimidazole drug with analgesic sedation properties. A sensitive and specific radioimmunoassay was developed for detomidine, 4(5)-(2,3-dimethylbenzyl)imidazole. The antibodies were raised in rabbits against a conjugate of detomidine and bovine thyroglobulin prepared by diazo reaction. Detomidine was iodinated with chloramine-T and immunoreactive tracer was purified in cation exchange chromatography. The sensitivity of the RIA was 1.6 fmol/tube allowing direct detomidine measurements from minute serum and urine samples (0.1-0.2 microliter) as well as tissue homogenates (10 microliters). For concentrations below 16 pmol/ml chloroform extraction wa...
Efficacy of four anthelmintics against benzimidazole-resistant cyathostomes of horses. In order to confirm benzimidazole resistance as recommended at a workshop of the Commission of the European Communities the isolate 'E' of cyathostome strongyles originating from a stud where benzimidazole resistance had been demonstrated by egg hatch tests and by egg count reduction tests was investigated in two series of critical tests. Each of 11 foals reared strongyle-free was infected with 130,000 third stage cyathostome larvae. One animal remained untreated, two pairs of foals were treated with paste formulations of the (pro)benzimidazoles cambendazole (20 mg/kg bodyweight) or febantel (...
Treatment of guttural pouch mycosis. Seventeen cases of guttural pouch mycosis (including two bilaterally affected cases) were diagnosed in a three year period. The presenting signs were, in order of frequency, epistaxis at rest, nasal catarrh, pharyngeal paralysis, ipsilateral laryngeal hemiplegia, swelling of the submandibular/parotid region, extension of the head and neck and dyspnoea. Ligation of the origin of the internal carotid and occipital arteries was attempted in 10 of the cases exhibiting epistaxis. Bilateral ligation was performed on one animal with an untoward sequelae. Where surgery was successfully completed furth...
Prevalence and control of benzimidazole-resistant small strongyles on German thoroughbred studs. The prevalence of benzimidazole-resistant small strongyles was determined in a survey, conducted on 14 thoroughbred studs, which compared the faecal egg counts of groups of horses before and after treatment with the recommended doses of cambendazole (20 mg kg-1 b.w.) or febantel (6 mg kg-1 b.w.). Benzimidazole-resistant cyathostomes were found on all farms examined. Pyrantel pamoate (19 mg kg-1 b.w.), oxibendazole (10 mg kg-1 b.w.) and ivermectin (0.2 mg kg-1 b.w.) reduced the strongyle egg counts on these studs by 97-100% at 2 weeks post-treatment. However, 6 weeks after dosing the reduction ...
Critical test and safety evaluations of an oral paste preparation of mebendazole and trichlorfon in horses. Critical tests were done on 24 naturally parasitized horses to compare the antiparasitic activity of an oral paste preparation of mebendazole and trichlorfon with that of the marketed powder formulation. Each formulation was administered at the recommended dosages of 8.8 mg of mebendazole and 40 mg of trichlorfon/kg of body weight. Efficacy of the paste formulation ranged from 97.7% to 100% against 2nd- and 3rd-stage Gasterophilus spp, adult Strongylus vulgaris, S edentatus, Parascaris equorum, small strongyles; and larval and adult forms of Oxyuris equi. Adverse effects were generally limited...
Analysis of pharmaceutical dosage forms for oxfendazole: II. Simultaneous liquid chromatographic determination of oxfendazole and trichlorfon in equine paste. A reverse phase liquid chromatographic procedure is described for the simultaneous determination of oxfendazole [2-(methoxycarbonylamino)-5-phenylsulfinylbenzimidazole] and trichlorfon [(2,2,2-trichloro-1-hydroxyethyl)phosphonic acid dimethyl ester] in equine paste. The sample is extracted by sonication in methanol. Insoluble excipients are removed by centrifugation and an aliquot plus internal standard are diluted with dilution solvent (water-acetonitrile-phosphoric acid, 80 + 20 + 1). The samples are filtered and injected onto a Partisil-5 ODS-3 column with acetonitrile-0.01 M phosphate buff...
Prevalence of benzimidazole-resistant small strongyles in horses in a southeastern Pennsylvania practice. A survey was conducted to determine the prevalence of benzimidazole (BZ)-resistant small strongyles in horses in a southeastern Pennsylvania practice. Resistant parasites were found in 291 of 342 horses surveyed. Anthelmintic practices and pasture management factors in use for 3 to 6 years did not correlate with the presence of resistant small strongyles. Benzimidazole-resistant small strongyles were recovered in horses that had been treated alternately with BZ and non-BZ products and in horses receiving BZ products as infrequently as twice a year. However, inasmuch as the horses may have been...
Use of oxibendazole for control of cambendazole-resistant small strongyles in a band of ponies: a six-year study. Oxibendazole (OBZ; 10 mg/kg of body weight) was administered to ponies at 8-week intervals to control strongylosis in a breeding band of Shetland-type ponies (n = 29 to 50) from October 1978 through September 1984. A similar use of cambendazole (CBZ; 20 mg/kg of body weight) in this band of ponies during the preceding 4-year period resulted in the survival of a CBZ-resistant population (S) of small strongyles. Effectiveness of OBZ treatments was monitored by pre- and posttreatment counts of the number of strongyle eggs per gram of feces (epg) and of the number of strongyle larvae per gram of f...
Evaluation of febantel used concurrently with piperazine citrate in horses. Fifty horses from a herd known to have benzimidazole-resistant small strongyles were treated with febantel (6 mg/kg), combinations of febantel (6 mg/kg) and piperazine citrate (25 or 55 mg base/kg), thiabendazole (44 mg/kg), or placebo (0.6 ml of water/kg). Pretreatment and 7-day posttreatment fecal examinations were done. Fecal cultures, strongyle egg per gram (epg) counts, sugar flotation fecal examinations, and in vitro testing for benzimidazole resistance were performed. Results of fecal examinations before treatment were similar in all horses, and results of testing were positive for benz...
The prevalence and intensity of internal parasites of horses in the U.S.A. Fifty-five adult horses were necropsied over a 15-month period, and their worm burdens counted and speciated. Twenty-one species of Cyathostominae were recovered. Ten species: Cyathostomum catinatum, Cylicocyclus nassatus, Cylicostephanus longibursatus, Cyathostomum coronatum, Cylicostephanus goldi, C. calicatus, C. minutus, Cylicocyclus leptostomus, C. insigne and Cyathostomum pateratum, comprised 98.9% of the total cyathostome burdens. These same 10 species also demonstrated high prevalences in 4 previous surveys. Eight of these 10 species have been shown to be resistant to benzimidazole ant...